R. Kikura-Hanajiri

2 papers in the library · publishing 2017-2019

Papers

Assessment of NMDA receptor inhibition of phencyclidine analogues using a high-throughput drebrin immunocytochemical assay.

Journal of pharmacological and toxicological methods September 1, 2019 Toshinari Mitsuoka, Kenji Hanamura, Noriko Koganezawa et al.

A high-throughput immunocytochemical assay using cultured rat hippocampal neurons can detect whether new psychoactive substances (NPS) inhibit NMDA receptor activity. Glutamate-induced reduction of drebrin cluster density along dendrites was competitively blocked by the NMDA receptor antagonist APV. The phencyclidine analogues PCP, 3-MeO-PCP, and 3-MeO-PCMo also antagonized the reduction, with IC50 values of 2.02 μM, 1.51 μM, and 26.67 μM respectively, indicating that 3-MeO-PCMo is less potent. The relative inhibitory potencies from IC50 values matched those from Ki values, suggesting the assay can estimate Ki for new PCP analogues without kinetic studies.

DOI: 10.1016/j.vascn.2019.106583 Full text Medicine Chemistry

Erratum to: The psychoactive drug 25B-NBOMe recapitulates rhabdomyolysis in zebrafish larvae

Forensic Toxicology January 1, 2017 G. Kawahara, Hideyuki Maeda, R. Kikura-Hanajiri et al. correction

The designer drug 25B-NBOMe, a potent agonist of the serotonin-2A (5-HT2A) receptor, causes lethal rhabdomyolysis in zebrafish larvae. Treatment with 25B-NBOMe reduced survival and locomotion, and altered skeletal muscle birefringence and immunostaining for dystroglycan and myosin heavy chain, consistent with rhabdomyolysis. This effect was blocked by the 5-HT2A receptor antagonists ritanserin and aripiprazole, but not by antagonists of other serotonin receptors, indicating a 5-HT2A-dependent mechanism. The 25B-NBOMe-treated zebrafish provides a useful model for studying rhabdomyolysis and screening therapeutic drugs.

DOI: 10.1007/s11419-017-0383-8 Full text Medicine Biology